NEW HYBRID STRUCTURES BASED ON MEMANTHINE AND EDARAVONE MOLECULES

V. V. Grigoriev; Григорьев В. В.; A. Yu. Aksinenko; Шевцова Е. Ф.; E. F. Shevtsova; Аксиненко А. Ю.; T. V. Goreva; Веселов И. М.; I. M. Veselov; Горева Т. В.; A. V. Gabrelyan; Габрельян А. В.; S. O. Bachurin; Бачурин С. О.

doi:10.31857/S2686738923600413

NEW HYBRID STRUCTURES BASED ON MEMANTHINE AND EDARAVONE MOLECULES

Autores: Grigoriev V.¹, Aksinenko A.¹, Shevtsova E.¹, Goreva T.¹, Veselov I.¹, Gabrelyan A.¹, Bachurin S.¹
Afiliações:
1. Institute of Physiologically Active Substances, Federal State Budgetary Institution of Science, Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences
Edição: Volume 512, Nº 1 (2023)
Páginas: 466-469
Seção: Articles
URL: https://journals.rcsi.science/2686-7389/article/view/140857
DOI: https://doi.org/10.31857/S2686738923600413
EDN: https://elibrary.ru/PYWTWG
ID: 140857

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Resumo
Sobre autores
Bibliografia
Arquivos suplementares
Estatísticas

Resumo

New hybrid structures based on memantine and edaravone molecules, in which the pyrazolone ring and adamantane fragments are linked by an alkyl linker, have been synthesized. It was found that in addition to the ability to block the intrachanal site of NMDA receptors, new hybrid compounds exhibit the property of blockers of the allosteric site of NMDA receptors, which is not inherent in memantine and edaravone preparations. The most active hit compound was determined, which, along with the properties of a two-site blocker of the NMDA receptor, exhibits a pronounced activity as an inhibitor of lipid peroxidation, similar to the drug edaravone.

Palavras-chave

amyotrophic lateral sclerosis, Alzheimer’s disease, memantine, edaravone, 1-aminoadamantanes, NMDA receptors, oxidative stress, lipid peroxidation

Bibliografia

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